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| 灯盏乙素衍生物的合成及抗大鼠心肌缺血活性研究 |
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杨丽梅1, 顾军2,3, 李建宇2,3, 代皓2, 李灵芝2,3
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1.天津医科大学药学院, 天津, 300070;2.武警医学院药物化学教研室, 天津, 300162;3.天津市职业与环境危害生物标志物重点实验室, 天津, 300162
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| 摘要: |
| [目的]设计合成一系列灯盏乙素衍生物并测试其保护大鼠缺血性心肌细胞活性,并初步探讨构效关系。[方法]以灯盏乙素为原料,将其水解后与卤代烷反应合成一系列灯盏乙素苷元的醚类衍生物;采用噻唑蓝(MTT)法测试化合物对缺氧损伤大鼠心肌细胞的保护作用。[结果]合成3个中间体及13个目标化合物,其中化合物2、4、5对缺氧损伤大鼠心肌细胞保护作用强于阳性对照药。[结论]灯盏乙素结构中糖基的有无对活性影响不大;4’位羟基为保护缺血大鼠心肌细胞的活性必须基团。 |
| 关键词: 灯盏乙素 合成 心肌缺血 构效关系 |
| DOI：10.11656/j.issn.1672-1519.2010.03.32 |
| 分类号: |
| 基金项目:国家自然科学基金项目(20902110);天津市自然科学基金项目(10JCYBJC14700) |
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| Synthesis of scutellarin derivatives and study of their anti-heart ischemia activities in rats |
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YANG Li-mei1, GU Jun2,3, LI Jian-yu2,3
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1.Pharmaceutial college, Tianjin Medical University, Tianjin 300070, China;2.Department of Pharmaceutical Chemistry, Medical Collage of Chinese People’s armed Police, Tianjin 300162, China;3.Tianjin Key Laboratory of Occupational and Environmental Hazards
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| Abstract: |
| [Objection] To design and synthesize a series of scutellarin derivatives for searching for their structure-activity relationship of protective effects on heart ischemia in Rats.[Methods] Using scutellarin as staring material,a series of ether derivatives based on scutellarein gained from scutellarin’s hydrolysis were synthesized by reacting with kinds of alkylogen,and then these compounds were evaluated for protective effects on Ischemic myocardial cells in Rats using MTT assay in vitro.[Results]The 3 intermediates and 13 target compounds were synthesized.The protection effect of compound 2,4,5 to ischemic myocardial cells in rats was better than the positive control.[Conclusion] The glucuronyl in the structure had little dedication on the activities of scutellarin while the 4’-OH was essential. |
| Key words: scutellarin synthesis heart ischemia structure-activity relationship |
